A ChE inhibitor that inhibits BChE and AChE (IC50s = 0.037 and 4.15 μM

Rivastigmine (tartrate) – 100 mg

Brand:
Cayman
CAS:
129101-54-8
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Rivastigmine is a cholinesterase (ChE) inhibitor that inhibits butyryl ChE (BChE) and acetyl ChE (AChE; IC50s = 0.037 and 4.15 μM, respectively).{24084} It increases levels of secreted amyloid precursor protein (sAPP) and decreases levels of soluble amyloid-β (1-40) and various N-terminal cleavage products in primary embryonic rat neurons undergoing degeneration when used at concentrations of 5 and 10 μM.{36871}. In a rat model of Alzheimer’s disease induced by aluminum chloride (AlCl3), rivastigmine (1 mg/kg per day) inhibits formation of amyloid plaques in brain sections and increases in AChE, IL-1β, and β-secretase 1 (BACE1) mRNA expression in the cerebral cortex.{36872} It inhibits AlCl3-induced increases in escape latency time in the Morris water maze in a rat model of Alzheimer’s disease when administered at a dose of 1 mg/kg. Rivastigmine (2 mg/kg) also reverses decreases in time spent in the open arms of an elevated plus maze, exploration time of a novel object in a novel object recognition test, and sucrose intake in a rat model of chronic mild stress.{36873} Formulations containing rivastigmine have been used in the treatment of dementia associated with Alzheimer’s disease and Parkinson’s disease.  

 

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A ChE inhibitor that inhibits BChE and AChE (IC50s = 0.037 and 4.15 μM, respectively); increases levels of sAPP and decreases levels of soluble amyloid-β (1-40) and various N-terminal cleavage products in primary embryonic rat neurons undergoing degeneration at 5 and 10 μM; inhibits formation of amyloid plaques in brain sections and increases in AChE, IL-1β, and BACE1 mRNA expression in the cerebral cortex at 1 mg/kg per day in a rat model of Alzheimer’s disease induced by AlCl3; inhibits AlCl3-induced increases in escape latency time in the Morris water maze in a rat model of Alzheimer’s disease at 1 mg/kg; reverses decreases in time spent in the open arms of an elevated plus maze, exploration time of a novel object in a novel object recognition test, and sucrose intake in a rat model of chronic mild stress at 2 mg/kg

Formal name: 3-[(1S)-1-(dimethylamino)ethyl]phenyl ester N-ethyl-N-methyl-carbamic acid, 2R,3R-dihydroxybutanedioate

Synonyms:  Exelon|SDZ-ENA 713

Molecular weight: 400.4

CAS: 129101-54-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Acetylcholine Turnover||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Behavioral Neuroscience|Depression||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease||Research Area|Neuroscience|Neuroprotection

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